SYNTHESIS AND QUANTITATIVE STRUCTURE ACTIVITY RELATIONSHIP (QSAR) STUDY OF NEW 3- ALLYL-5-SUBSTITUTED-3,4,5,6-TETRAHYDRO-2H-1,3,5- THIADIAZINE-2-THIONES OF A POTENTIAL ANTIMICROBIAL ACTIVITY | ||||
| Bulletin of Pharmaceutical Sciences Assiut University | ||||
| Article 3, Volume 30, Issue 1, June 2007, Page 39-50 PDF (206.85 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/bfsa.2007.63543 | ||||
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| Authors | ||||
| Alaa M. Hayallah; Awwad A. Radwan* | ||||
| Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut-71527, Egypt | ||||
| Abstract | ||||
| Fifteen new 3-allyl-5-substituted-3,4,5,6-tetrahydro-2H-1,3,5- thiadiazine-2-thiones were synthesized by the reaction of allylamine with carbon disulfide and potassium hydroxide, followed by formaldehyde and appropriate primary amine such as alkyl, aralkylamines, glycine, L-alanine or ethyl glycine ester. The title compounds were tested, in vitro, for antimicrobial activity against gram-positive bacteria (Bacillus cereus, Staphylococcus aureus, Micrococcus leuteus), Gram-negative bacteria (Escherichia coli, Serratia marcescens, Pseudomonas aeruginosa), and some fungi (Aspergillus flavus, Aspergillus niger, candida albicans, Geotrichum candidum, Scopulariopsis brevicaulis and Trichophyton rubrum), using agar disc method. Quantitative structure activity relationship study was performed using the log form of MIC against Scopulariopsis brevicaulis fungi and some physicochemical descriptors (MR, L, and Fr) of substituents at N-5 position. The log MIC were found to be negatively linearly correlated with MR and L and positively linearly correlated with Fr. | ||||
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